Consumer medicine information

Setear

Betahistine dihydrochloride

BRAND INFORMATION

Brand name

Setear

Active ingredient

Betahistine dihydrochloride

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Setear.

What is in this leaflet

This leaflet answers some common questions about Setear tablets. It does not contain all the available information. It does not take the place of talking to your doctor and pharmacist.

If you have any concerns about being given this medicine, ask your doctor or pharmacist.

All medicines have risks and benefits. Your doctor has weighed the risks of you being given Setear tablets against the benefits this medicine is expected to have for you.

Keep this leaflet with the medicine. You may need to read it again.

What Setear is used for

Setear is used to treat a disorder of the working of your inner ear. This disorder may include one or more of the following symptoms, in one or both ears:

  • Ringing in the ears (tinnitus)
  • Loss of clear hearing
  • Problems with balance (vertigo)

These symptoms may also be associated with nausea, vomiting and headache. Often these symptoms together are referred to as Méniere's Syndrome.

Setear tablets contain the active ingredient betahistine dihydrochloride, which work by improving the blood flow of the inner ear and restoring it to normal. It also acts on the nerve endings in the inner ear to normalize the way in which the nerves respond to outside influences.

Your doctor may have prescribed Setear for another reason. Ask your doctor if you have any questions about why Setear has been prescribed for you.

There is no evidence that Setear is addictive.

This medicine is available only with a doctor’s prescription.

Before you take Setear

When you must not take it

Do not take Setear if:

  • you are pregnant or intend to become pregnant. Setear may affect your developing baby if taken during pregnancy.
  • you are breast-feeding or plan to breast-feed. Setear may pass into breast milk and therefore there is possibility that the breast-fed baby may be affected.
  • you are allergic to betahistine dihydrochloride or any of the ingredients listed at the end of this leaflet. Some symptoms of an allergic reaction include skin rash, itching, shortness of breath or swelling of the face, lips or tongue, which may cause difficulty in swallowing or breathing.
  • you have a rare abnormality of the adrenal gland known as phaeochromochytoma.
  • you have or have had a peptic ulcer.

Do not give Setear to children under 18 years of age.

Do not take Setear after the expiry date (EXP) printed on the pack.

Do not take Setear if the packaging is torn or shows signs of tampering, or if the tablets do not look quite right. If it has expired or is damaged, return it to your pharmacist for disposal.

If you are not sure whether you should start taking Setear, talk to your doctor or pharmacist.

Before you start to take it

You must tell your doctor if you have allergies to:

  • any other medicines
  • any other substances, such as foods, preservatives or dyes

Tell your doctor if:

  • you have or have had a peptic ulcer,
  • you suffer from asthma
  • you have a history of allergic skin conditions or if you have or have had any other medical conditions.

Tell your doctor if you are pregnant or intend to become pregnant. Your doctor will discuss the possible risks and benefits of using Setear during pregnancy.

Tell your doctor if you are breastfeeding or plan to breast-feed. Your doctor will discuss the possible risks and benefits of using Setear during breastfeeding.

If you have not told your doctor about any of the above, tell them before you start taking Setear.

Taking other medicines

Tell your doctor if you are taking any other medicines, including medicines you buy without a prescription from your pharmacy, supermarket or health food shop.

Some medicines and Setear may interfere with each other. These include:

  • any antihistamine medications, which are used to treat allergies and allergic reactions
  • monoamine oxidase inhibitors (MAOIs) (e.g. some antidepressants, selegiline)

These medicines may be affected by Setear or may affect how well it works. You may need different amounts of your medicine, or you may need to take different medicines. Your doctor will advise you.

Your doctor and pharmacist may have more information on medicines to be careful with or avoid while taking Setear.

How take Setear

Follow all directions given to you by your doctor or pharmacist carefully. They may differ from the information contained in this leaflet.

Your doctor or pharmacist will tell you how many tablets you will need to take each day. This depends on your condition and whether or not you are taking any other medicines.

If you do not understand the instructions on the box, ask your doctor or pharmacist for help.

How much to take

The usual adult starting dose is one tablet taken twice a day. However your doctor may prescribe a different dose depending on the severity of your condition.

The maximum recommended daily dosage is 48 mg.

How to take it

Swallow Setear with a glass of water.

When to take it

Take Setear at about the same time each day.

Taking your tablets at the same time each day will have the best effect. It will also help you remember when to take the tablets.

Take Setear during or immediately after a meal, at about the same time each day. If you take Setear on an empty stomach, it may cause stomach upsets.

How long to take it

If you follow your doctor's instructions Setear should start working within a few days, although in some cases it may take a few weeks. The length of time that you should take Setear tablets varies from patient to patient. Some people respond rapidly to treatment and others may take some time. Please be patient with your treatment and take your tablets regularly. Do not stop taking your medicine unless your doctor tells you to - even if you feel better.

If you forget to take your tablets

If it is almost time for your next dose, skip the dose you missed and take your next dose when you are meant to.

Otherwise, take it as soon as you remember, and then go back to taking your medicine as you would normally.

Do not take a double dose to make up for the dose that you missed. This may increase the chance of you getting an unwanted side effect.

If you are not sure what to do, ask your doctor or pharmacist.

If you have trouble remembering to take your medicine, ask your pharmacist for some hints.

If you take too much (overdose)

Immediately contact your doctor or pharmacist or the Poisons Information Centre (In Australia, call 13 11 26), or go to Accident and Emergency at the nearest hospital, if you think that you or anyone else may have taken too much Setear. Do this even if there are no signs of discomfort or poisoning.

The most common symptom of overdosing is nausea.

While you are taking Setear

Things you must do

Tell any other doctors, dentists, and pharmacists who are treating you that you are taking Setear.

If you are about to be started on any new medicine, tell your doctor, dentist or pharmacist that you are taking Setear.

If you plan to have surgery that needs a general anaesthetic, tell your doctor or dentist that you are taking Setear.

If you become pregnant while taking Setear, tell your doctor immediately.

Keep all of your doctor's appointments so that your progress can be checked. Your doctor may do some tests from time to time to make sure the medicine is working and to prevent unwanted side effects.

Things you must not do

Do not give Setear to anyone else, even if they have the same condition as you.

Do not take Setear to treat any other complaints unless your doctor tells you to.

Do not stop taking Setear, or lower the dosage without checking with your doctor.

Side Effects

Tell your doctor or pharmacist as soon as possible if you do not feel well while you are taking Setear. All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side-effects.

Ask your doctor or pharmacist to answer any questions you may have.

Following is a list of possible side effects. Do not be alarmed by this list.

You may not experience any of them.

If you get any side effects, do not stop taking Setear without first talking to your doctor.

Tell your doctor or pharmacist if you notice any of the following and they worry you:

  • skin irritations
  • stomach upsets
  • dizziness
  • fast heart beat
  • headache
  • difficulty sleeping (insomnia)
  • tiredness
  • nausea, vomiting, bloating, or swollen stomach
  • diarrhoea

These side effects are usually mild and often short-lived. Some symptoms may also be present as part of your disorder. Stomach upsets can be overcome by taking Setear during meals.

Tell your doctor as soon as possible if you notice any of the following:

  • skin reactions
  • difficulty breathing
  • convulsions
  • hallucinations
  • confusion
  • allergic reaction
  • low blood pressure, slow heart beat

These may be serious side effects. You may need medical attention. Serious side effects are very rare.

Other side effects not listed above may occur in some patients. Tell your doctor or pharmacist if you notice anything that is making you feel unwell.

After using Setear

Storage

Keep your tablets in the pack until it is time to take them. If you take the tablets out of the pack they will not keep well.

Keep your tablets in a cool, dry place where the temperature stays below 25°C. Do not store Setear or any other medicine in the bathroom or near a sink.

Do not leave it on a windowsill or in the car on hot days. Heat and dampness can destroy some medicines.

Keep Setear tablets where children cannot reach them. A locked cupboard at least one-and- a-half metres above the ground is a good place to store medicines.

Disposal

If your doctor tells you to stop taking Setear, or the tablets have passed their expiry date, ask your pharmacist what to do with any tablets left over.

Product description

What the tablets look like

Setear tablets are white and flat with beveled edges. They have a breakline on one side. Available in packs of 60 tablets.

Ingredients

Active ingredient:

Setear 24 mg tablet - 24 mg betahistine dihydrochloride.

Inactive ingredients:

  • lactose monohydrate
  • maize starch
  • microcrystalline cellulose
  • citric acid
  • povidone
  • crospovidone
  • hydrogenated vegetable oil

Contains sugars as lactose.

Supplier/ Distributor

Southern Cross Pharma Pty Ltd
Suite 5/118 Church Street
Hawthorn VIC 3122

This leaflet was prepared in February 2020.

Australian Register Number
24 mg tablet: AUST R 261439 (blisters)

Published by MIMS April 2020

BRAND INFORMATION

Brand name

Setear

Active ingredient

Betahistine dihydrochloride

Schedule

S4

 

Notes

Distributed by Southern XP Pty Ltd

1 Name of Medicine

Betahistine dihydrochloride.

2 Qualitative and Quantitative Composition

Setear tablets contain the active ingredient betahistine dihydrochloride.
Each Setear tablet contains 24 mg of betahistine dihydrochloride.

Excipient with known effect.

Sugars as lactose.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Setear 24 mg tablets are white flat tablets with bevelled edges and a break line on one side.

4 Clinical Particulars

4.1 Therapeutic Indications

Meniere's syndrome as defined by the following core symptoms: vertigo (with nausea/vomiting); hearing loss (hardness of hearing); tinnitus.

4.2 Dose and Method of Administration

The recommended starting dose in adults is one 24 mg taken two times a day.
The maximum recommended daily dosage is 48 mg, which may be taken as 16 mg three times daily or 24 mg twice daily. Refer to separate Product Information for betahistine 16 mg tablets.
The tablets may be taken with or without food. However, if gastrointestinal upset occurs, it is recommended that the tablets be taken with meals.
The dosage should be individually adapted according to the response. Improvement in symptoms may be observed in the first few days to weeks of treatment.

4.3 Contraindications

During pregnancy and lactation;
in children less than 18 years;
in patients suffering from phaeochromocytoma;
in patients with active peptic ulcer or a history of this condition;
in patients with hypersensitivity to any component to the product (see Section 6.1 List of Excipients).

4.4 Special Warnings and Precautions for Use

Patients with bronchial asthma need to be carefully monitored during therapy.
Caution should be taken in the treatment of patients receiving antihistamines (see Section 4.5 Interactions with Other Medicines and Other Forms of Interactions).

Use in the elderly.

No data available.

Paediatric use.

Due to lack of clinical experience, betahistine dihydrochloride should not be used in children less than 18 years (see Section 4.3 Contraindications).

Effects on laboratory tests.

Interactions with laboratory tests have not been established.

4.5 Interactions with Other Medicines and Other Forms of Interactions

In vitro data indicate an inhibition of betahistine metabolism by drugs that inhibit monoamine-oxidase (MAO) including MAO subtype B (e.g. selegiline). Caution is recommended when using betahistine and MAO inhibitors (including MAO-B selective) concomitantly.
An antagonism between betahistine dihydrochloride and antihistamines could be expected on a theoretical basis. However, no such interactions have been reported.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

Studies in animals are inadequate or may be lacking, but available data show no evidence of an increased occurrence of foetal damage.
(Category B2)
Betahistine dihydrochloride should not be used during pregnancy (see Section 4.3 Contraindications), since there are insufficient data on the use of this drug during pregnancy to evaluate possible harmful effects.
Studies in animals are inadequate or may be lacking, but available data show no evidence of an increased occurrence of foetal damage.
 Betahistine dihydrochloride should not be used during lactation (see Section 4.3 Contraindications).

4.7 Effects on Ability to Drive and Use Machines

Betahistine is indicated for Meniere's syndrome defined by the triad of core symptoms vertigo, hearing loss and tinnitus which can negatively affect the ability to drive and use machines. In a small clinical study of healthy volunteers specifically designed to investigate the ability to drive, betahistine had no or negligible effects compared to placebo.

4.8 Adverse Effects (Undesirable Effects)

Most of the reported adverse reactions pertain to the skin, gastrointestinal tract, body as a whole, nervous system, respiratory system and cardiovascular system.
Events are listed within body systems and categorised by frequency according to the following definitions:
Common (frequency greater than or equal to 1 and < 10%); Uncommon (frequency greater than or equal to 0.1% and < 1%); Rare (frequency greater than or equal to 0.01% and < 0.1%); Very rare (frequency < 0.01%).

Skin and subcutaneous tissue disorders.

Rare: various types of rash, pruritus and urticaria/angioneurotic oedema. These reactions are probably related to the histamine-like structure of betahistine. There was a single case of Stevens-Johnson syndrome.

Body as a whole.

Rare: tiredness and malaise.

Gastrointestinal system.

Common: nausea and dyspepsia. Rare: vomiting, diarrhoea, abdominal distension, bloating and epigastric pain have been reported. These symptoms were usually mild. Gastrointestinal disturbances may be relieved by reducing the dose or by taking betahistine with meals.

Nervous system.

Common: headache. Rare: dizziness. Very rare: convulsions, somnolence, confusion and hallucinations.
Some of these symptoms may also be observed as part of the disease condition and are usually resolved without changes to the treatment schedule.
Patients with neurological events usually presented with confounding factors.

Cardiovascular system.

Very rare: vasodilation, postural hypotension and tachycardia.

Respiratory system.

Very rare: dyspnoea, asthma and bronchospasms (see Section 4.4 Special Warnings and Precautions for Use).

Immune system disorder.

Hypersensitivity reactions, e.g. anaphylaxis have been reported.

Reporting suspected adverse events.

Reporting suspected adverse reactions after registration of the medical product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions at http://www.tga.gov.au/reporting-problems.

4.9 Overdose

Symptoms.

There have been a few cases of overdosage reported. Although in most cases no overdose symptoms were reported, some patients have experienced mild to moderate symptoms of overdosage including nausea, dry mouth, epigastric pain and sleepiness at doses above 200 mg. A case of convulsion was reported at a dose of 728 mg. In all cases recovery was complete.

Treatment.

Treatment should include standard supportive measures.
For information on the management of overdose, contact the Poisons Information Centre on 131126 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

The mechanism of action of betahistine is not known. Pharmacological testing in animals has shown that the blood circulation in the striae vascularis of the inner ear improves, probably by means of a relaxation of the precapillary sphincters of the microcirculation of the inner ear.
In further animal pharmacological studies, betahistine was found to have weak H1-receptor agonistic and considerable H3-antagonistic properties in the CNS and autonomic nervous system. Betahistine was also found to have a dose dependent inhibiting effect on spike generation of neurons in lateral and medial vestibular nuclei in cats. The importance of this observation in the action against Meniere's syndrome or vestibular vertigo, however, remains unclear.

Clinical trials.

Twice versus three times daily dosage administration.

Four published studies comparing the safety and efficacy of betahistine 48 mg daily, when administered in twice daily or three times daily regimens have been assessed.
Tran Ba Huy 1992 was a randomized, controlled, open label study comparing the safety and efficacy of betahistine administered as 24 mg twice daily or 16 mg three times daily for 3 months, in 24 patients with recurrent vertigo, with or without cochlear symptoms typical of Meniere's disease.
Gananca 2009 was a randomized, open label study comparing the efficacy and tolerability of betahistine, administered either as 16 mg three times daily (60 patients) or 24 mg twice daily (60 patients) for 24 weeks, when used to treat vertigo in patients with well-established Meniere's disease.
Benecke 2010 was a prospective, multicentre, open label comparative post-marketing surveillance study comparing the effect on quality of life and tolerability of betahistine, administered either as 16 mg three times daily (742 patients) or 24 mg twice daily (1226 patients) for 3 months, when used to treat vertigo of peripheral vestibular origin just 13.3% with a diagnosis of Meniere's. Treatment allocation to each treatment regimen was determined by the approved product information of each country contributing patients to the study, and therefore was not randomly assigned.
Jurkiewicz 2009 was a prospective, open-label, parallel group trial which compared the efficacy of betahistine, when administered in a twice daily (44 patients) or three times daily dosage (38 patients) regimen, to treat patients with balancing disorders or vertigo. The maximum daily dosing regimens were administered for 4 weeks only, prior to reducing the dosage regimens to 12 mg twice daily and 8 mg three times daily for the remaining 8 weeks' of the study. Assignment to either regimen was not strictly randomized, but rather based on a pre-treatment screening questionnaire and examination undertaken by an audiology specialist.
All studies were conducted in a patient population relevant to the approved indication. The efficacy of the two dosage regimens was evaluated using a range of primary and secondary outcome measures. Efficacy measures were assessed at baseline and at least twice during the course of the treatment period. Outcomes were assessed subjectively by investigator and/or the individual patient. Jurkiewicz 2009 also objectively assessed efficacy using videonystagmography and posturography.
The subjective measures ranged from changes in vertigo intensity, severity, frequency and duration of vertigo, dizziness handicap index to health related quality of life (QoL), global assessment of progression of vertigo. The objective measures assessed posture, movement and optokinetics.
In all studies both treatment arms produced significant improvements in the various efficacy parameters during the treatment periods.
With the small patient numbers no statistically significant difference between the twice daily and three times daily regimens was demonstrated in any study.
There was no difference in the incidence or range of adverse events reported in the 3 studies which evaluated safety, between the twice daily and three times daily dosage regimens.

5.2 Pharmacokinetic Properties

Absorption.

In humans, orally administered doses of betahistine dihydrochloride are rapidly and completely absorbed from the gastrointestinal tract.

Metabolism.

The drug is rapidly metabolised to one major metabolite, 2-pyridylacetic acid, and excreted in the urine. Studies with radiolabelled betahistine have demonstrated a plasma half-life of 3.4 hours and a urinary half-life of 3.5 hours for the radiolabel.

Excretion.

Urinary excretion of the label was about 90% complete within 24 hours of administration.

5.3 Preclinical Safety Data

Genotoxicity.

No nonclinical data are available on the genotoxic potential of betahistine.

Carcinogenicity.

No animal data are available on the carcinogenic potential of betahistine.

6 Pharmaceutical Particulars

6.1 List of Excipients

Setear 24 mg tablets contain the following inactive ingredients: lactose monohydrate, maize starch, microcrystalline cellulose, citric acid, crospovidone, povidone and hydrogenated vegetable oil.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG). The expiry date can be found on the packaging.

6.4 Special Precautions for Storage

Store below 25°C.

6.5 Nature and Contents of Container

Setear 24 mg tablets are available in PVC/PE/PVDC/Al blister packs of 25*, 60 tablets and a sample pack of 15 tablets.
*Not marketed.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of by taking to your local pharmacy.

6.7 Physicochemical Properties

Chemical structure.


Chemical name: 2-[2-methylamino)ethyl]pyridine dihydrochloride.
Molecular formula: C8H12N2.2HCl.
Molecular weight: 209.1.

CAS number.

5579-84-0.
Betahistine dihydrochloride is a white almost white crystalline powder which is very hygroscopic. The product is very soluble in water, freely soluble in methanol and 96% ethanol, and slightly soluble in isopropanol. The pKa values are 3.5 and 9.7.
Chemically, betahistine has a close resemblance to histamine.

7 Medicine Schedule (Poisons Standard)

S4 (Prescription Only Medicine).

Summary Table of Changes